Epaldeudomide

CAS 1918159-31-5

MF C25H252HFN3O5, MW 468.5 g/mol

(3S)-3-deuterio-3-[7-[[2-fluoro-4-(morpholin-4-ylmethyl)phenyl]methoxy]-3-oxo-1H-isoindol-2-yl]piperidine-2,6-dione

(3S)-3-[4-[[2-Fluoro-4-(4-morpholinylmethyl)phenyl]methoxy]-1,3-dihydro-1-oxo-2H-isoindol-2-yl]-2,6-piperidinedione-3-d

KPG-818, KPG 818, ANTINEOPLASTIC, KV0TBL8MUS

Epaldeudomide (also known as KPG-818) is an investigational, next-generation immunomodulatory drug and “molecular glue” developed by Kangpu Biopharmaceuticals. Designed as a targeted therapy, it works by binding to the CRL4-CRBN E3 ubiquitin ligase complex to degrade specific proteins, showing promise in treating blood cancers, solid tumors, and autoimmune diseases.

Mechanism of Action

• Molecular Glue: It is a small molecule that acts as a modulator of the cereblon (CRBN) E3 ligase.
• Protein Degradation: It targets and induces the rapid degradation of two Ikaros zinc-finger transcription factors: IKZF3 (Aiolos) and IKZF1 (Ikaros).
• Immunomodulation: By degrading these targets, epaldeudomide triggers broad-spectrum immune responses, reduces tumor proliferation, and suppresses inflammation (such as the production of TNF-\(\alpha \)).

Therapeutic Pipeline and Research

Epaldeudomide is currently undergoing clinical evaluation to assess its safety, tolerability, and efficacy.

• Hematology/Oncology: It is being studied for the treatment of hematologic malignancies (such as multiple myeloma and lymphomas). It demonstrates potent anti-tumor and anti-angiogenic activity without several severe side effects typically associated with earlier immunomodulatory drugs.
• Autoimmune and Inflammatory Disorders: Because of its broad anti-inflammatory effects and ability to inhibit TNF-\(\alpha \), it is being explored for use against autoimmune conditions and inflammatory arthritis.

• OriginatorKangpu Biopharmaceuticals
• ClassAnti-inflammatories; Antineoplastics; Small molecules
• Mechanism of ActionCRBN protein modulators; Ubiquitin protein ligase complex modulators
• Phase IIInflammatory bowel diseases
• Phase I/IISystemic lupus erythematosus
• Phase IHaematological malignancies
• PreclinicalBehcet’s syndrome; Crohn’s disease; Multiple myeloma
• 06 Dec 2025Efficacy, pharmacokinetics and adverse events data from a phase I trial in Haematological malignancies presented at 67th American Society of Hematology Annual Meeting and Exposition (ASH-Hem-2025)
• 26 Nov 2025Epaldeudomide is still in phase I trials for Haematological malignancies (Second-line therapy or greater) in USA (PO, Capsule) (NCT04283097)
• 18 Nov 2025Efficacy and adverse events data from a phase I trial in Haematological malignancies released by Kangpu Biopharmaceuticals

SYN

US-10017492-B2
US-20170313676-A1

SYN

EP-3643709-A1
EP-3643709-B1
https://patentscope.wipo.int/search/en/detail.jsf?docId=EP293972088&_cid=P21-MPEVL7-37300-1

Example 37: Compound A382

[0196]  3-(4-((2-fluoro-5-(3-morpholinopropoxy)benzyl)amino)-1-oxoisoindolin-2-yl)piperidine-2,6-dione, A382.

[0197]  ¹H NMR (DMSO- d ₆, 300 MHz): δ 11.00 (s, 1H), 7.32 (t, J = 7.8 Hz, 1H), 7.22 (t, J = 7.8 Hz, 1H), 7.05-7.13 (m, 2H), 6.93 (d, J = 7.5 Hz, 1H), 6.64 (d, J = 7.8 Hz, 1H), 6.28 (t, J = 6.3 Hz, 1H), 5.07-5.13 (m, 1H), 4.38 (d, J= 5.7 Hz, 2H), 4.28 (d, J= 17.4 Hz, 1H), 4.16 (d, J= 17.4 Hz, 1H), 3.54 (t, J= 4.5 Hz, 4H), 3.42 (s, 2H), 2.85-2.97 (m, 1H), 2.57-2.63 (m, 1H), 2.26-2.38 (m, 5H), 2.00-2.09 (m, 1H). LCMS: 467.2 ([M+1] ⁺).

Example 69: Compound A406

[0296]  ( S)-3-deuterium-3-(4-((2-fluoro-4-(morpholinomethyl)benzyl)oxy)-1-oxoisoindolin-2-yl)piperidine-2,6-dione, A406.

[0297]  ¹H NMR (DMSO- d ₆, 300 MHz): δ 10.98 (s, 1H),7.47-7.55 (m, 2H), 7.31-7.38 (m, 2H), 7.16-7.20 (m, 2H), 5.24 (s, 2H), 5.06-5.12 (m, 0.04H), 4.35 (d, J = 18.0 Hz, 1H), 4.19 (d, J = 18.0 Hz, 1H), 3.55 (br, 4H), 3.47 (s, 2H), 2.82-2.94 (m, 1H), 2.48-2.57 (m, 1H), 2.33-2.42 (m, 5H), 1.91-1.96 (m, 1H). LCMS: 469.2 ([M+1] ⁺).

ADVT

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References

• Isoindoline derivative, intermediate, preparation method, pharmaceutical composition and use thereofPublication Number: US-10017492-B2Priority Date: 2014-10-30Grant Date: 2018-07-10
• Isoindoline derivative, intermediate, preparation method, pharmaceutical composition and use thereofPublication Number: EP-3643709-A1Priority Date: 2014-10-30
• Isoindoline derivative, intermediate, preparation method, pharmaceutical composition and use thereofPublication Number: US-2017313676-A1Priority Date: 2014-10-30
• Isoindoline derivative, intermediate, preparation method, pharmaceutical composition and use thereofPublication Number: EP-3643709-B1Priority Date: 2014-10-30Grant Date: 2021-10-20

/////////epaldeudomide, ANAX LABS, KPG-818, KPG 818, ANTINEOPLASTIC, KV0TBL8MUS